entecavir ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals carbocyclic nucleosides 1019 142217-69-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • entecavir monohydrate
  • anhydrous entecavir
  • BMS-200475-01
  • entecavir
  • baraclude
  • entecavir hydrate
Entecavir, a guanosine nucleoside analogue with activity against HBV reverse transcriptase, is efficiently phosphorylated to the active triphosphate form, which has an intracellular half-life of 15 hours. By competing with the natural substrate deoxyguanosine triphosphate, entecavir triphosphate functionally inhibits all three activities of the HBV reverse transcriptase: (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA. Entecavir triphosphate is a weak inhibitor of cellular DNA polymerases alpha, beta, and delta and mitochondrial DNA polymerase gamma with Ki values ranging from 18 to > 160 microM.
  • Molecular weight: 277.28
  • Formula: C12H15N5O3
  • CLOGP: -1.78
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 4
  • TPSA: 125.76
  • ALOGS: -1.63
  • ROTB: 2

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.50 mg O

ADMET properties:

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Drug Use | Suggest Off label Use Form| |View source of the data|




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

External reference:

Pharmaceutical products:

entecavir